Therapeutic Formulation Patent – US 8669292

US Patent – Grant: 8,669,292
Publication Date: March 11, 2014

Compositions and formulations demonstrate positive effects against a broad variety of cancer, autoimmune diseases, viruses and provides antioxidant protection against peroxyl hydrophilic, peroxyl lipophilic, hydroxyl, peroxynitrite and superoxide radicals, which can be used for nutritional and nutraceutical uses, and used as dietary supplements.

Abstract

The invention provides compositions and formulations comprising catechol and/or acetogenins and various combinations thereof; including various combinations with other ingredients including botanical preparations containing acetogenin, an extract of green tea or a therapeutically active flavanoid contained in green tea; and one or more quinones. The invention includes a pharmaceutical composition including a salt of rhodizonic acid, an OH anion-generating base, a non-toxic acid, a quinone, a salt-containing sulfite, catechol and optionally, an acetogenin and an extract of green tea. The compositions and formulations demonstrate positive effects against a broad variety of cancer, autoimmune diseases, viruses and provides antioxidant protection against peroxyl hydrophilic, peroxyl lipophilic, hydroxyl, peroxynitrite and super oxide radicals. The compositions and formulations can be used for nutritional and nutraceutical uses, and used as dietary supplements.

Summary of the Invention

In one aspect, the invention provides a composition for the treatment of cancer, rheumatic disorder, or autoimmune disorder; or for scavenging free radicals, comprising a therapeutically effective amount of a chemical having the form:

Screen Shot 2014-06-12 at 10.00.06 AM

wherein the composition is formulated as a tablet, a capsule, a time release tablet, a time release capsule; a time release pellet; a sublingual tablet; a gel capsule; a microencapsulation; a transdermal delivery formulation; a transdermal gel; a transdermal patch; a sterile solution; a sterile solution prepared for use as an intramuscular or subcutaneous injection, for use as a direct injection into a targeted site, or for intravenous administration; a solution prepared for rectal administration; a solution prepared for administration through a gastric feeding tube or duodenal feeding tube; a suppository for rectal administration; a liquid for oral consumption prepared as a solution or an elixir; a topical cream; a gel; a lotion; a tincture; a syrup; an emulsion; or a suspension; except that wherein the composition is formulated as a liquid for oral consumption prepared as a solution or an elixir, catechol is the only active ingredient.

In a second aspect, the invention provides a composition for the treatment of cancer, rheumatic disorder, or autoimmune disorder; or for scavenging free radicals, the composition consisting essentially of therapeutically effective amounts of a first ingredient consisting of a chemical having the form:

Screen Shot 2014-06-12 at 10.00.06 AM

and at least one second ingredient selected from the group consisting of: an anti-neoplastic in the form of acetogenin or a botanical preparation that comprises an anti-neoplastic in the form of acetogenin; an extract of green tea or a therapeutically active flavanoid contained in green tea; and a quinone selected from the group consisting of tetrahydroxyquinone and sulfites of tetrahydroxyquinone.

In a third aspect, the invention provides a composition for the treatment of cancer, rheumatic disorder, or autoimmune disorder; or for scavenging free radicals, the composition consisting essentially of therapeutically effective amounts of a chemical having the form: an anti-neoplastic in the form of acetogenin; an extract of green tea; and a quinone selected from the group consisting of tetrahydroxyquinone and sulfites of tetrahydroxyquinone.

In a fourth aspect, the invention provides a composition for the treatment of cancer, rheumatic disorder, or autoimmune disorder; or for scavenging free radicals, the composition comprising therapeutically effective amounts of a first ingredient consisting of a chemical having the form:

Screen Shot 2014-06-12 at 10.00.06 AM

and at least one second ingredient selected from the group consisting of:

a) an anti-neoplastic in the form of acetogenin or a botanical preparation that comprises an anti-neoplastic in the form of acetogenin;

b) an extract of green tea or a therapeutically active flavanoid contained in green tea; and

c) a quinone selected from the group consisting of tetrahydroxyquinone and sulfites of tetrahydroxyquinone;

wherein the composition is formulated as a dry powder or granules, a tablet, a capsule, a time release tablet, a time release capsule; a time release pellet, a sublingual tablet; a gel capsule; a microencapsulation; a transdermal delivery formulation; a transdermal gel; a transdermal patch; a sterile solution; a sterile solution prepared for use as an intramuscular or subcutaneous injection, for use as a direct injection into a targeted site, or for intravenous administration; a solution prepared for rectal administration; a solution prepared for administration through a gastric feeding tube or duodenal feeding tube; a suppository for rectal administration; a liquid for oral consumption prepared as a solution or an elixir; a topical cream; a gel; a lotion; a tincture; a syrup; an emulsion; or a suspension;
except that wherein the composition does not comprise at least one second ingredient selected from the group consisting of: b) and c), then the composition is not formulated as a liquid for oral consumption prepared as a solution or an elixir.

In a fifth aspect, the invention provides composition for the treatment of cancer, rheumatic disorder, or autoimmune disorder; or for scavenging free radicals, the composition comprising therapeutically effective amounts of a chemical having the form:

Screen Shot 2014-06-12 at 10.00.06 AM

and at least one quinone selected from the group consisting of tetrahydroxyquinone, hexahydrabenzene, rhodizonic acid, triquinol, triquinoyl, leuconic acid and a sulfite of tetrahydroxyquinone, hexahydrabenzene, rhodizonic acid, triquinol, triquinoyl or leuconic acid; and an acid selected from the group consisting of croconic acid and a sulfite of croconic acid; wherein the composition is formulated as a dry powder or granules, a tablet, a capsule, a time release tablet, a time release capsule; a time release pellet, a time release pellet; a sublingual tablet; a gel capsule; a microencapsulation; a transdermal delivery formulation; a transdermal gel; a transdermal patch; a sterile solution; a sterile solution prepared for use as an intramuscular or subcutaneous injection, for use as a direct injection into a targeted site, or for intravenous administration; a solution prepared for rectal administration; a solution prepared for administration through a gastric feeding tube or duodenal feeding tube; a suppository for rectal administration; a topical cream; a gel; a lotion; a tincture; a syrup; an emulsion; or a suspension.

In a sixth aspect, the invention provides a composition for the treatment of cancer, rheumatic disorder, or autoimmune disorder; or for scavenging free radicals, the composition comprising a therapeutically effective amount of an antineoplastic in the form of acetogenin, wherein the composition is formulated as a time release tablet, a time release capsule; a time release pellet, a transdermal delivery formulation; a transdermal gel; a transdermal patch; a sterile solution; a sterile solution prepared for use as an intramuscular or subcutaneous injection, for use as a direct injection into a targeted site, or for intravenous administration; a solution prepared for rectal administration; a solution prepared for administration through a gastric feeding tube or duodenal feeding tube; or a suppository for rectal administration.

In a further aspect, the invention provides methods for treatment of cancer, rheumatic disorder, or autoimmune disorder; or for scavenging free radicals in a mammal including a human, comprising administering a composition set forth in the first, second, third, fourth, fifth, or sixth aspect of the invention; or a combination thereof.

In a particular aspect, the invention provides a method for treatment of cancer, rheumatic disorder, or autoimmune disorder; or for scavenging free radicals in a mammal including a human, comprising administering a therapeutically effective amount of a chemical having the form:

Screen Shot 2014-06-12 at 10.00.06 AM

wherein the composition is formulated as a tablet, a capsule, a time release tablet, a time release capsule; a time release pellet; a sublingual tablet; a gel capsule; a microencapsulation; a transdermal delivery formulation; a transdermal gel; a transdermal patch; a sterile solution; a sterile solution prepared for use as an intramuscular or subcutaneous injection, for use as a direct injection into a targeted site, or for intravenous administration; a solution prepared for rectal administration; a solution prepared for administration through a gastric feeding tube or duodenal feeding tube; a suppository for rectal administration; a liquid for oral consumption prepared as a solution or an elixir; a topical cream; a gel; a lotion; a tincture; a syrup; an emulsion; or a suspension.
with that wherein said composition is formulated as a liquid for oral consumption prepared as a solution or an elixir, catechol is the only active ingredient.

The invention further encompasses methods for nutritional supplementation, dietary supplementation, food supplementation, nutraceutical administration or nutra-therapeutical administration in a subject including a human, comprising orally administering a composition set forth in the first, second, third, fourth, fifth, or sixth aspect of the invention; or a combination thereof.

The invention further provides the described compositions formulated as time release pellets, and/or dry powder or granules; as described in further detail below. Particular embodiments of the present invention include a food preparation, a time release pellet, and/or dry powder or granules set forth in various formulations of the inventive compositions. Thus, it is recognized that the present composition can be administered as a food or pet food additive, and the invention encompasses such food preparations comprising the time release pellets and/or dry powder or granules. The invention further encompasses methods of administering the food preparations of the present invention to a subject.

Particular compositions of the present invention generally include any therapeutically effective combination of a salt of rhodizonic acid and an OH anion-generating base (resulting in croconic acid), a non-toxic acid, a quinone, a salt-containing sulfite, catechol, an acetogenin, and an extract of green tea or any of the therapeutically effective components of green tea including catechin, epicatechin, epicatechin gallate, epigallocatechin, epigallocatechin gallate or other similar compounds such as flavone, myricetin, quercitin, or rutin. The invention includes inventive administrative forms (formulations) necessary to improve efficacy, dosage compliance, convenience, aesthetics and appeal.

The compositions of the present invention overcomes the failings of known compositions and methods of disease treatments by providing a composition that is high in antioxidants, is safe to produce, and is adaptable to administration to a patient without the undesirable appeal problems associated with the known compositions and methods. The compositions are more efficacious against disease states and health damaging species of free radicals.

The compositions can be characterized as an oral medicament, a nutritional supplement, a dietary supplement, a food supplement, a food additive, a pharmaceutical, a nutraceutical, or a nutratherapeutical composition, and the invention encompasses providing the compositions as such.

The compositions of the present invention are strong antioxidants. They are also effective against a broad variety of cancer(s), autoimmune and rheumatoid diseases such as lupus and rheumatoid arthritis and many viruses. The present composition is herein shown to be an effective antioxidant that works on the major forms of the oxygen-related species of free radicals, including the peroxyl (hydrophilic and lipophilic), hydroxyl, peroxynitrite and super oxide radicals. It is also believed that the compositions of the present invention has utility in reducing the side effects of radiation therapy and chemotherapy, as well as in radio-sensitizing tumors; thus improving the efficacy of radiation therapy.

The compositions of the present invention also overcome the problems commonly associated with the production of the known nutratherapeutical compositions by the effective elimination of the noxious fumes. This results in improved laboratory conditions and ease of maintenance of proper conditions. The invention encompasses methods of producing the inventive compositions described herein, including the methods particularly set forth and/or provided below by way of example.

The present invention also improves the efficacy of the known nutratherapeutical formulas against tumors, by providing chronic cytotoxic dosing of tumors, and by providing a more consistent supply of antioxidants in the bloodstream, thereby providing a more effective in-vivo method of destroying the pernicious oxygen species of free radicals that are implicated in over 50 disease states.

As a further improvement over the art, the various compositions of the present invention may achieve superior efficacies without the use of such components as copper, potassium, triquinoyl, leuconic acid, hexahydrabenzene and rhodozonic acid. The absence of these components, while improving the effectiveness of the various compositions of the present invention, further supports the effectiveness of the unique approach described herein. By avoiding such extra components, possible adverse patient reactions and cost can be reduced. Improvement is also achieved by adding other synergistic components, which yield superior antioxidant and anticancer properties such as acetogenins, an extract of green tea which is high in flavanoids such as catechin, epicatechin, epicatechin gallate, epigallocatechin, epigallocatechin gallate or other similar compounds such as flavone, myricetin, quercitin, or rutin.

Whether comprised of the identical ingredients of the known composition Cantron or comprised of the superior components of the new compositions described herein, the new administrative forms (formulations) of the invention represent a significant improvement over the oral liquid form that has been solely employed for decades as they improve efficacy, dosage compliance, convenience, aesthetics and appeal by removing the characteristic adverse taste, burning of mouth tissues and other such disadvantages. The new forms change the characteristics of the known composition dramatically and these vastly superior properties represent a new and significant invention.

Other advantages and features of the present invention will become apparent from the following detailed description and appended claims.

References:
USPTO: 8669292
Download: PDF